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Further studies on bis-charged tetraazacyclophanes as potent inhibitors of small conductance Ca(2+)-activated K+ channels.
Yang D, Arifhodzic L, Ganellin CR, Jenkinson DH.
Eur J Med Chem. 2013 May;63:907-23. doi: 10.1016/j.ejmech.2013.02.029. Epub 2013 Mar 6.
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The pharmacology of cimetidine, a new histamine H2-receptor antagonist. 1975.
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Br J Pharmacol. 2010 Jul;160 Suppl 1:S52-3. doi: 10.1111/j.1476-5381.2010.00854.x. No abstract available.
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Molecular features of the prazosin molecule required for activation of Transport-P.
da Silva JF, Walters M, Al-Damluji S, Ganellin CR.
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Synthesis of novel ketoconazole derivatives as inhibitors of the human Pregnane X Receptor (PXR; NR1I2; also termed SXR, PAR).
Das BC, Madhukumar AV, Anguiano J, Kim S, Sinz M, Zvyaga TA, Power EC, Ganellin CR, Mani S.
Bioorg Med Chem Lett. 2008 Jul 15;18(14):3974-7. doi: 10.1016/j.bmcl.2008.06.018. Epub 2008 Jun 10.
Synthesis and pharmacological testing of polyaminoquinolines as blockers of the apamin-sensitive Ca2+-activated K+ channel (SK(Ca)).
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Bioorg Med Chem. 2007 Aug 15;15(16):5457-79. Epub 2007 May 26.
BF2.649 [1-{3-[3-(4-Chlorophenyl)propoxy]propyl}piperidine, hydrochloride], a nonimidazole inverse agonist/antagonist at the human histamine H3 receptor: Preclinical pharmacology.
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J Pharmacol Exp Ther. 2007 Jan;320(1):365-75. Epub 2006 Sep 27.
Enhancement of hippocampal pyramidal cell excitability by the novel selective slow-afterhyperpolarization channel blocker 3-(triphenylmethylaminomethyl)pyridine (UCL2077).
Shah MM, Javadzadeh-Tabatabaie M, Benton DC, Ganellin CR, Haylett DG.
Mol Pharmacol. 2006 Nov;70(5):1494-502. Epub 2006 Jul 28.
Histamine and its receptors.
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Br J Pharmacol. 2006 Jan;147 Suppl 1:S127-35.
Partial structures of ketoconazole as modulators of the large conductance calcium-activated potassium channel (BK(Ca)).
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Inhibitors of tripeptidyl peptidase II. 3. Derivation of butabindide by successive structure optimizations leading to a potential general approach to designing exopeptidase inhibitors.
Ganellin CR, Bishop PB, Bambal RB, Chan SM, Leblond B, Moore AN, Zhao L, Bourgeat P, Rose C, Vargas F, Schwartz JC.
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Search for the pharmacophore in prazosin for Transport-P.
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Search for histamine H3 receptor antagonists with combined inhibitory potency at Ntau-methyltransferase: ether derivatives.
Apelt J, Grassmann S, Ligneau X, Pertz HH, Ganellin CR, Arrang JM, Schwartz JC, Schunack W, Stark H.
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Search for histamine H(3) receptor ligands with combined inhibitory potency at histamine N-methyltransferase: omega-piperidinoalkanamine derivatives.
Grassmann S, Apelt J, Ligneau X, Pertz HH, Arrang JM, Ganellin CR, Schwartz JC, Schunack W, Stark H.
Arch Pharm (Weinheim). 2004 Oct;337(10):533-45.
Bis-quinolinium cyclophanes: toward a pharmacophore model for the blockade of apamin-sensitive SKCa channels in sympathetic neurons.
Galanakis D, Ganellin CR, Chen JQ, Gunasekera D, Dunn PM.
Bioorg Med Chem Lett. 2004 Aug 16;14(16):4231-5.
Defining determinant molecular properties for the blockade of the apamin-sensitive SKCa channel in guinea-pig hepatocytes: the influence of polarizability and molecular geometry.
Galanakis D, Ganellin CR.
Bioorg Med Chem Lett. 2004 Aug 2;14(15):4031-5.
Meta-substituted aryl(thio)ethers as potent partial agonists (or antagonists) for the histamine H3 receptor lacking a nitrogen atom in the side chain.
Pelloux-Léon N, Fkyerat A, Piripitsi A, Tertiuk W, Schunack W, Stark H, Garbarg M, Ligneau X, Arrang JM, Schwartz JC, Ganellin CR.
J Med Chem. 2004 Jun 3;47(12):3264-74.
4-(omega-(alkyloxy)alkyl)-1H-imidazole derivatives as histamine H(3) receptor antagonists/agonists.
Meier G, Krause M, Hüls A, Ligneau X, Pertz HH, Arrang JM, Ganellin CR, Schwartz JC, Schunack W, Stark H.
J Med Chem. 2004 May 6;47(10):2678-87.
Structural variations of 1-(4-(phenoxymethyl)benzyl)piperidines as nonimidazole histamine H3 receptor antagonists.
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The sleep lipid oleamide may represent an endogenous anticonvulsant: an in vitro comparative study in the 4-aminopyridine rat brain-slice model.
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Inhibition of the antigen-induced activation of RBL-2H3 cells by cetiedil and some of its analogues.
Narenjkar J, Assem el-SK, Ganellin CR.
Eur J Pharmacol. 2004 Jan 12;483(2-3):107-16.
The sleep inducing brain lipid cis-oleamide (cOA) does not modulate serotonergic transmission in the CA1 pyramidal neurons of the hippocampus in vitro.
Neuropharmacology. 2004 Jan;46(1):63-73.
Protean agonism at histamine H3 receptors in vitro and in vivo.
Gbahou F, Rouleau A, Morisset S, Parmentier R, Crochet S, Lin JS, Ligneau X, Tardivel-Lacombe J, Stark H, Schunack W, Ganellin CR, Schwartz JC, Arrang JM.
Proc Natl Acad Sci U S A. 2003 Sep 16;100(19):11086-91. Epub 2003 Sep 5.
Therapeutic implications of constitutive activity of receptors: the example of the histamine H3 receptor.
Schwartz JC, Morisset S, Rouleau A, Ligneau X, Gbahou F, Tardivel-Lacombe J, Stark H, Schunack W, Ganellin CR, Arrang JM.
J Neural Transm Suppl. 2003;(64):1-16. Review.
Imidazole derivatives as a novel class of hybrid compounds with inhibitory histamine N-methyltransferase potencies and histamine hH3 receptor affinities.
Grassmann S, Apelt J, Sippl W, Ligneau X, Pertz HH, Zhao YH, Arrang JM, Ganellin CR, Schwartz JC, Schunack W, Stark H.
Bioorg Med Chem. 2003 May 15;11(10):2163-74.
Novel nonimidazole histamine H3 receptor antagonists: 1-(4-(phenoxymethyl)benzyl)piperidines and related compounds.
Mikó T, Ligneau X, Pertz HH, Ganellin CR, Arrang JM, Schwartz JC, Schunack W, Stark H.
J Med Chem. 2003 Apr 10;46(8):1523-30.
Influence of bulky substituents on histamine h(3) receptor agonist/antagonist properties.
Sasse A, Ligneau X, Rouleau A, Elz S, Ganellin CR, Arrang JM, Schwartz JC, Schunack W, Stark H.
J Med Chem. 2002 Aug 29;45(18):4000-10.
Tritylamino aromatic heterocycles and related carbinols as blockers of ca 2+-activated potassium ion channels underlying neuronal hyperpolarization.
Zunszain PA, Shah MM, Miscony Z, Javadzadeh-Tabatabaie M, Haylett DG, Ganellin CR.
Arch Pharm (Weinheim). 2002 Apr;335(4):159-66.
Piperidino-hydrocarbon compounds as novel non-imidazole histamine H(3)-receptor antagonists.
Meier G, Ligneau X, Pertz HH, Ganellin CR, Schwartz JC, Schunack W, Stark H.
Bioorg Med Chem. 2002 Aug;10(8):2535-42.
Progress in the proxifan class: heterocyclic congeners as novel potent and selective histamine H(3)-receptor antagonists.
Grassmann S, Sadek B, Ligneau X, Elz S, Ganellin CR, Arrang JM, Schwartz JC, Stark H, Schunack W.
Eur J Pharm Sci. 2002 May;15(4):367-78.
Development of a new class of nonimidazole histamine H(3) receptor ligands with combined inhibitory histamine N-methyltransferase activity.
Apelt J, Ligneau X, Pertz HH, Arrang JM, Ganellin CR, Schwartz JC, Schunack W, Stark H.
J Med Chem. 2002 Feb 28;45(5):1128-41.
Importance of the lipophilic group in carbamates having histamine H3-receptor antagonist activity.
Kieć-Kononowicz K, Wiecek M, Sasse A, Ligneau X, Elz S, Ganellin CR, Schwartz JC, Stark H, Schunack W.
Pharmazie. 2000 May;55(5):349-55.
The histamine H3 receptor and its ligands.
Stark H, Arrang JM, Ligneau X, Garbarg M, Ganellin CR, Schwartz JC, Schunack W.
Prog Med Chem. 2001;38:279-308. Review. No abstract available.
Synthesis and structure-activity relationships of cetiedil analogues as blockers of the Ca(2+)-activated K+ permeability of erythrocytes.
Roxburgh CJ, Ganellin CR, Athmani S, Bisi A, Quaglia W, Benton DC, Shiner MA, Malik-Hall M, Haylett DG, Jenkinson DH.
J Med Chem. 2001 Sep 27;44(20):3244-53.
Influence of imidazole replacement in different structural classes of histamine H(3)-receptor antagonists.
Meier G, Apelt J, Reichert U, Grassmann S, Ligneau X, Elz S, Leurquin F, Ganellin CR, Schwartz JC, Schunack W, Stark H.
Eur J Pharm Sci. 2001 Jun;13(3):249-59.
Different antagonist binding properties of human and rat histamine H3 receptors.
Stark H, Sippl W, Ligneau X, Arrang JM, Ganellin CR, Schwartz JC, Schunack W.
Bioorg Med Chem Lett. 2001 Apr 9;11(7):951-4.
Calcium-activated potassium channels sustain calcium signaling in T lymphocytes. Selective blockers and manipulated channel expression levels.
Fanger CM, Rauer H, Neben AL, Miller MJ, Rauer H, Wulff H, Rosa JC, Ganellin CR, Chandy KG, Cahalan MD.
J Biol Chem. 2001 Apr 13;276(15):12249-56. Epub 2001 Jan 22.
Benzophenone derivatives and related compounds as potent histamine H3-receptor antagonists and potential PET/SPECT ligands.
Sasse A, Ligneau X, Sadek B, Elz S, Pertz HH, Ganellin CR, Arrang JM, Schwartz JC, Schunack W, Stark H.
Arch Pharm (Weinheim). 2001 Feb;334(2):45-52.
Medicinal chemistry in the development of societies. Biodiversity and natural products.
Monge A, Chorghade M, Erhardt PW, Ganellin CR, Koga N, Lindberg P, Perun TJ, Topliss JG, Trivedi BK, Wermuth CG.
Eur J Med Chem. 2000 Dec;35(12):1121-5.
Clotrimazole analogues: effective blockers of the slow afterhyperpolarization in cultured rat hippocampal pyramidal neurones.
Shah MM, Miscony Z, Javadzadeh-Tabatabaie M, Ganellin CR, Haylett DG.
Br J Pharmacol. 2001 Feb;132(4):889-98.
Anesthetic-like interaction of the sleep-inducing lipid oleamide with voltage-gated sodium channels in mammalian brain.
Nicholson RA, Zheng J, Ganellin CR, Verdon B, Lees G.
Anesthesiology. 2001 Jan;94(1):120-8. Erratum in: Anesthesiology 2001 Apr;94(4):723.
High constitutive activity of native H3 receptors regulates histamine neurons in brain.
Morisset S, Rouleau A, Ligneau X, Gbahou F, Tardivel-Lacombe J, Stark H, Schunack W, Ganellin CR, Schwartz JC, Arrang JM.
Nature. 2000 Dec 14;408(6814):860-4.
Distinct pharmacology of rat and human histamine H(3) receptors: role of two amino acids in the third transmembrane domain.
Ligneau X, Morisset S, Tardivel-Lacombe J, Gbahou F, Ganellin CR, Stark H, Schunack W, Schwartz JC, Arrang JM.
Br J Pharmacol. 2000 Dec;131(7):1247-50.
Analogues and derivatives of ciproxifan, a novel prototype for generating potent histamine H3-receptor antagonists.
Stark H, Ligneau X, Sadek B, Ganellin CR, Arrang JM, Schwartz JC, Schunack W.
Bioorg Med Chem Lett. 2000 Oct 16;10(20):2379-82.
Novel histamine H(3)-receptor antagonists with carbonyl-substituted 4-(3-(phenoxy)propyl)-1H-imidazole structures like ciproxifan and related compounds.
Stark H, Sadek B, Krause M, Hüls A, Ligneau X, Ganellin CR, Arrang JM, Schwartz JC, Schunack W.
J Med Chem. 2000 Oct 19;43(21):3987-94.
bis-Quinolinium cyclophanes: 8,14-diaza-1,7(1, 4)-diquinolinacyclotetradecaphane (UCL 1848), a highly potent and selective, nonpeptidic blocker of the apamin-sensitive Ca(2+)-activated K(+) channel.
Chen JQ, Galanakis D, Ganellin CR, Dunn PM, Jenkinson DH.
J Med Chem. 2000 Sep 21;43(19):3478-81. No abstract available.
New histamine H(3)-receptor ligands of the proxifan series: imoproxifan and other selective antagonists with high oral in vivo potency.
Sasse A, Sadek B, Ligneau X, Elz S, Pertz HH, Luger P, Ganellin CR, Arrang JM, Schwartz JC, Schunack W, Stark H.
J Med Chem. 2000 Aug 24;43(17):3335-43.
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